Ibrutinib

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ibrutinib

 (i-BROO-tih-nib)A drug used to treat chronic lymphocytic leukemia, small lymphocytic lymphoma, and Waldenstrom macroglobulinemia (a type of non-Hodgkin lymphoma). It is also used to treat mantle cell lymphoma and marginal zone lymphoma in patients who have received at least one other treatment. It is also being studied in the treatment of other types of cancer. Ibrutinib blocks a protein called Bruton’s tyrosine kinase (BTK), which may help keep cancer cells from growing. It is a type of tyrosine kinase inhibitor. Also called Imbruvica.

Information about Ibrutinib

Ibrutinib is an oral inhibitor of Bruton’s tyrosine kinase that is used in the therapy of refractory chronic lymphocytic leukemia (CLL) and mantle cell lymphoma.   

Liver safety of Ibrutinib

Ibrutinib has not been associated with serum enzyme elevations during therapy, but has been linked to rare cases of clinically apparent acute liver injury and to reactivation of hepatitis B. 

== Mechanism of action of Ibrutinib ==  Ibrutinib (eye broo’ ti nib) is an orally available, small molecule inhibitor of Bruton’s tyrosine kinase (BTK), which is an essential component in the B cell receptor signaling pathway.  Inhibition of this pathway prevents B cell activation, differentiation and proliferation.  Deficiency of BTK is the cause of X linked (Bruton’s) agammaglobulinemia, and B cell receptor signaling through BTK has been shown to be critical for proliferation and survival of malignant B lymphocytes in mantle cell lymphoma and CLL. 

FDA approval information for Ibrutinib

Ibrutinib was approved for use in the United States as therapy for refractory mantle cell lymphoma in 2013 and for refractory CLL in 2014.  Subsequently, it has been approved for use in Waldenstrom's macroglobulinemia, marginal zone lymphoma and chronic graft versus host disease after failure of standard therapy. 

Dosage and administration for Ibrutinib

Ibrutinib is available in capsules of 70 and 140 mg and as tablets of 140, 280, 420 and 560 mg under the brand name Imbruvica.  The recommended dose is 420 (CLL) or 540 (lymphoma) mg orally, once daily. 

Side effects of Ibrutinib

Side effects are common, but usually mild-to-moderate in severity; they include myelosuppression, fatigue, diarrhea, nausea, vomiting, anorexia, constipation, peripheral edema, dyspnea, arthralgia, myalgia, rash and fever.  Uncommon, but potentially serious side effects include severe bone marrow suppression, infections, bleeding, cardiac arrhythmias, hypertension, tumor lysis syndrome and embryo-fetal toxicity.

 


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